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STELLA MARIA CASCIOFERRO

Pyrazolo[3,4-d]pyrimidine Derivatives as COX-2 Selective Inhibitors: Synthesis and Molecular Modelling Studies

  • Authors: Raffa, D; Maggio, B; Plescia, F; Cascioferro, SM; Raimondi, MV; Plescia, S; Cusimano, MG
  • Publication year: 2009
  • Type: Articolo in rivista (Articolo in rivista)
  • Key words: COX-2 inhibitors; Docking, Pyrazolo[3,4-d]pyrimidine; 4(3H)-Quinazolinone
  • OA Link: http://hdl.handle.net/10447/38966

Abstract

The pyrazolo[3,4-d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4-d]pyrimidin- 4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5- benzamido-1H-pyrazolo[3,4-d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5- aminopyrazole-4(N-benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a–d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Molecular modelling studies confirmed the obtained biological results.